本研究系统探索了金骨止痛凝胶(JGZTG)功能性物质的透皮扩散规律。采用自动透皮(干热)采样系统,通过单因素试验研究了JGZTG的透皮扩散研究方法。建立了高效液相色谱法(HPLC)测定阿魏酸含量的方法,senkyunolideI,肉桂酸,羟基-ε-黄氧精,羟基-α-黄霉素,在JGZTG的透皮扩散溶液中和羟基-β-黄氧精。研究了成分在16h内的透皮扩散规律。结果表明,JGZTG的最佳透皮扩散方法如下:以大鼠皮肤为透皮屏障;以生理盐水为接受介质;JGZTG的剂量为0.3g,并用乙酸乙酯萃取接收溶液。透皮扩散结果表明,阿魏酸的释放,肉桂酸,senkyunolideI在0-8h显着增加,在8-16h减慢。药物释放是一个扩散和溶解的协同过程,其中阿魏酸和肉桂酸遵循Higuchi和Ritger-Peppas方程,利古拉内酯一世遵循Higuchi方程。羟基-ε-zanthoxylin的透皮扩散曲线,羟基-α-zanthoxylin,羟基-β-zanthoxylin在16小时内连续释放,药物释放为骨架溶解。扩散定律遵循零阶方程,一阶方程,还有Ritger-Peppas方程.在clonclusion中,它是阿魏酸的控释,乙丙酮I,肉桂酸,羟基-ε-吡咯烷酮,羟基-α-吡咯烷酮,和羟基-β-吡咯二甲酚在JGZTG中,可以在16小时内保持稳定的血药浓度,12h各组分的累积透过率可以达到24h累积透过率的80%,这符合BIS在死亡的临床用药规律。
This study systematically explored the transdermal diffusion law of functional substances of Jingu Zhitong Gel(JGZTG). The transdermal diffusion research methods of JGZTG were investigated by single factor trial with the automated transdermal(dry-heat) sampling system. High performance liquid chromatography(HPLC) content determination method was established to determine the contents of ferulic acid, senkyunolide I, cinnamic acid, hydroxy-ε-xanthoxylin, hydroxy-α-xanthoxylin, and hydroxy-β-xanthoxylin in the transdermal diffusion solution of JGZTG. The transdermal diffusion law of the components within 16 h was investigated. The results showed that the optimal transdermal diffusion method of JGZTG was as follows: Rat skin was used as the transdermal barrier; normal saline was used as the receiving medium; the dosage of JGZTG was 0.3 g, and the receiving solution was extracted by ethyl acetate. The results of transdermal diffusion showed that the release of ferulic acid, cinnamic acid, and senkyunolide I increased significantly at 0-8 h and slowed down at 8-16 h. The drug release was a synergic process of diffusion and dissolution, in which ferulic acid and cinnamic acid followed Higuchi and Ritger-Peppas equations, and liguolactone I followed Higuchi equation. The transdermal diffusion curves of hydroxy-ε-zanthoxylin, hydroxy-α-zanthoxylin, and hydroxy-β-zanthoxylin showed continuous release within 16 h, and the drug release was skeleton dissolution. The diffusion law followed zero-order equation, first-order equation, and Ritger-Peppas equation. In clonclusion, it is a controlled release of ferulic acid, ligustrone I, cinnamic acid, hydroxy-ε-pyrroxylin, hydroxy-α-pyrroxylin, and hydroxy-β-pyrroxylin in JGZTG, which can maintain stable blood drug concentration with 16 h, and the cumulative transmittance of each component with 12 h can reach 80% of cumulative transmittance with 24 h, which is in line with the clinical drug use law of bis in die.